JWH-133 [Ligand Id: 747] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL371214 (JWH-133) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Displacement of human recombinant CB1 receptor expressed in HEK293 cell membranes incubated for 90 mins by Cheng-Prusoff equation based analysis | B | 5 | pKi | >10000 | nM | Ki | Medchemcomm (2014) 5: 1571-1576 |
| ChEMBL | Displacement of [3H]-CP-55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by beta-counting analysis | B | 6 | pKi | >1000 | nM | Ki | Eur J Med Chem (2019) 165: 347-362 [PMID:30583970] |
| ChEMBL | Binding affinity to cannabinoid CB1 receptor | B | 6.17 | pKi | 677 | nM | Ki | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB1 receptor in cell free system | B | 6.17 | pKi | 677 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| ChEMBL | Binding affinity to CB1 receptor | B | 6.17 | pKi | 677 | nM | Ki | Bioorg Med Chem (2011) 19: 5698-5707 [PMID:21872477] |
| ChEMBL | Displacement of [3H]CP55,940 from human recombinant CB1 receptor expressed in HEK293 cell membranes after 90 mins | B | 6.17 | pKi | 677 | nM | Ki | Eur J Med Chem (2014) 74: 524-532 [PMID:24518874] |
| ChEMBL | Displacement of [3H]CP-55,940 from human recombinant CB1R expressed in HEK-293 cells after 90 mins by liquid scintillation counting | B | 6.17 | pKi | 677 | nM | Ki | J Med Chem (2014) 57: 8777-8791 [PMID:25272206] |
| ChEMBL | Displacement of [3H]CP55,940 from human recombinant CB1 receptor expressed in HEK293 cell membranes after 90 mins | B | 6.17 | pKi | 677 | nM | Ki | Eur J Med Chem (2015) 90: 526-536 [PMID:25486424] |
| ChEMBL | Displacement of [3H]-CP-55940 from recombinant human CB1 receptor overexpressed in HEK293 cell membranes after 90 mins | B | 6.17 | pKi | 677 | nM | Ki | Eur J Med Chem (2015) 97: 10-18 [PMID:25935384] |
| ChEMBL | Binding affinity to CB1 receptor | B | 6.17 | pKi | 677 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells | B | 6.17 | pKi | 677 | nM | Ki | J Med Chem (2009) 52: 3644-3651 [PMID:19435366] |
| ChEMBL | Displacement of [3H]CP55940 from recombinant human CB1 receptor expressed in human HEK293 cell membrane after 90 mins | B | 6.93 | pKi | 116.8 | nM | Ki | Eur J Med Chem (2012) 52: 284-294 [PMID:22483967] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
| ChEMBL | Displacement of human recombinant CB1 receptor expressed in HEK293 cell membranes incubated for 90 mins by radioligand binding assay | B | 5 | pIC50 | >10000 | nM | IC50 | Medchemcomm (2014) 5: 1571-1576 |
| CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746] | ||||||||
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in DBA/J2 mouse brain | B | 6.34 | pKi | 458 | nM | Ki | J Med Chem (2006) 49: 5947-5957 [PMID:17004710] |
| CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat brain membranes after 1 hr by liquid scintillation spectrophotometry | B | 6.17 | pKi | 677 | nM | Ki | Bioorg Med Chem (2010) 18: 7809-7815 [PMID:20943404] |
| ChEMBL | Binding affinity to rat CB1 receptor | B | 6.17 | pKi | 677 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor | F | 5.7 | pEC50 | 1995.26 | nM | EC50 | J Med Chem (2006) 49: 554-566 [PMID:16420041] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Displacement of human recombinant CB2 receptor expressed in HEK293 cell membranes incubated for 90 mins by Cheng-Prusoff equation based analysis | B | 6.85 | pKi | 140 | nM | Ki | Medchemcomm (2014) 5: 1571-1576 |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor | B | 7.69 | pKi | 20.3 | nM | Ki | J Med Chem (2006) 49: 70-79 [PMID:16392793] |
| ChEMBL | Displacement of [3H]-CP-55940 from human CB2 receptor expressed in CHO cell membranes after 1 hr by beta-counting analysis | B | 8.1 | pKi | 8 | nM | Ki | Eur J Med Chem (2019) 165: 347-362 [PMID:30583970] |
| ChEMBL | Binding affinity to CB2 receptor | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
| ChEMBL | Binding affinity to cannabinoid CB2 receptor | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells after 1 hr by liquid scintillation spectrophotometry | B | 8.47 | pKi | 3.4 | nM | Ki | Bioorg Med Chem (2010) 18: 7809-7815 [PMID:20943404] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB2 receptor in cell free system | B | 8.47 | pKi | 3.4 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| ChEMBL | Binding affinity to CB2 receptor | B | 8.47 | pKi | 3.4 | nM | Ki | Bioorg Med Chem (2011) 19: 5698-5707 [PMID:21872477] |
| ChEMBL | Binding affinity to human CB2 receptor | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation spectrometric method | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| GtoPdb | - | - | 8.5 | pKi | 3.16 | nM | Ki |
Bioorg Med Chem (1999) 7: 2905-14 [PMID:10658595]; Expert Opin Investig Drugs (2000) 9: 1553-71 [PMID:11060760] |
| ChEMBL | Displacement of [3H]-CP-55940 from recombinant human CB2 receptor overexpressed in HEK293 cell membranes after 90 mins | B | 8.52 | pKi | 3 | nM | Ki | Eur J Med Chem (2015) 97: 10-18 [PMID:25935384] |
| ChEMBL | Displacement of [3H]CP-55,940 from human recombinant CB2R expressed in HEK-293 cells after 90 mins by liquid scintillation counting | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2014) 57: 8777-8791 [PMID:25272206] |
| ChEMBL | Displacement of [3H]CP55,940 from human recombinant CB2 receptor expressed in HEK293 cell membranes after 90 mins | B | 8.52 | pKi | 3 | nM | Ki | Eur J Med Chem (2015) 90: 526-536 [PMID:25486424] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2009) 52: 3644-3651 [PMID:19435366] |
| ChEMBL | Displacement of [3H]CP55,940 from human recombinant CB2 receptor expressed in HEK293 cell membranes after 90 mins | B | 8.52 | pKi | 3 | nM | Ki | Eur J Med Chem (2014) 74: 524-532 [PMID:24518874] |
| ChEMBL | Displacement of [3H]CP55940 from recombinant human CB2 receptor expressed in human HEK293 cell membrane after 90 mins | B | 8.74 | pKi | 1.82 | nM | Ki | Eur J Med Chem (2012) 52: 284-294 [PMID:22483967] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor | B | 10.64 | pKi | 0.02 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
| ChEMBL | Displacement of human recombinant CB2 receptor expressed in HEK293 cell membranes incubated for 90 mins by radioligand binding assay | B | 6.26 | pIC50 | 550 | nM | IC50 | Medchemcomm (2014) 5: 1571-1576 |
| ChEMBL | Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins by HTRF assay | F | 7.09 | pIC50 | 81.8 | nM | IC50 | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| ChEMBL | Agonist activity at recombinant human CB2R expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels after 30 mins by chemiluminescent detection based cAMP Hunter assay | F | 6.41 | pEC50 | 391.1 | nM | EC50 | J Med Chem (2020) 63: 7369-7391 [PMID:32515588] |
| ChEMBL | Effect on [35S]GTP-gamma-S binding to human CB2 receptor | F | 6.84 | pEC50 | 145.6 | nM | EC50 | J Med Chem (2006) 49: 70-79 [PMID:16392793] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 1.5 hrs by liquid scintillation spectrophotometry | F | 8.4 | pEC50 | 4 | nM | EC50 | Bioorg Med Chem (2010) 18: 7809-7815 [PMID:20943404] |
| CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936] | ||||||||
| ChEMBL | Displacement of [3H]CP-55940 from CB2 receptor in DBA/J2 mouse spleen | B | 7.19 | pKi | 65 | nM | Ki | J Med Chem (2006) 49: 5947-5957 [PMID:17004710] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
